Résumé
OBJECTIVE: To study the tissue distribution of doxorubicin-loaded cholesterol-modified glycol chitosan nanoparticles (named as DCN-16) in S180-bearing mice. METHODS: After intravenous administration of doxorubicin (DOX) or DCN-16, DOX concentrations in plasma and tissues samples which were collected at predetermined time were determined by high performance liquid chromatography (HPLC). And DOX distribution and targeting performance in vivo were evaluated. RESULTS: DCN-16 displayed long circulation time in S180-bearing mice. The area under the curve (AUC0-∞) of DCN-16 was lower in heart (P < 0.05), lung (P < 0.05) and kidney (P < 0.05) than that of free DOX. In addition, compared with free DOX, DCN-16 also produced significantly increased drug accumulation in liver (P < 0.05), spleen (P < 0.05) and tumor (P < 0.05). The relative tissue exposure (Re) of DCN-16 in tumor was 2.56-folds of free DOX. CONCLUSION: Encapsulating DOX with cholesterol-modified glycol chitosan nanoparticles can prolong the systemic circulation time of DOX, increase its anti-tumor targeting activity and reduce its cardiac toxicity.